EP2627181A4 - Heteroaryle und verwendungen davon - Google Patents

Heteroaryle und verwendungen davon

Info

Publication number
EP2627181A4
EP2627181A4 EP11833402.8A EP11833402A EP2627181A4 EP 2627181 A4 EP2627181 A4 EP 2627181A4 EP 11833402 A EP11833402 A EP 11833402A EP 2627181 A4 EP2627181 A4 EP 2627181A4
Authority
EP
European Patent Office
Prior art keywords
heteroaryls
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP11833402.8A
Other languages
English (en)
French (fr)
Other versions
EP2627181A2 (de
Inventor
Brian S Freeze
Masaaki Hirose
Hong Myung Lee
Todd B Sells
Zhan Shi
Leo R Takaoka
Stepan Vyskocil
Tianlin Xu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Millennium Pharmaceuticals Inc
Original Assignee
Millennium Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45938970&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP2627181(A4) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium Pharmaceuticals Inc filed Critical Millennium Pharmaceuticals Inc
Publication of EP2627181A2 publication Critical patent/EP2627181A2/de
Publication of EP2627181A4 publication Critical patent/EP2627181A4/de
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
EP11833402.8A 2010-10-13 2011-10-13 Heteroaryle und verwendungen davon Withdrawn EP2627181A4 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39251510P 2010-10-13 2010-10-13
PCT/US2011/056135 WO2012051410A2 (en) 2010-10-13 2011-10-13 Heteroaryls and uses thereof

Publications (2)

Publication Number Publication Date
EP2627181A2 EP2627181A2 (de) 2013-08-21
EP2627181A4 true EP2627181A4 (de) 2014-03-19

Family

ID=45938970

Family Applications (1)

Application Number Title Priority Date Filing Date
EP11833402.8A Withdrawn EP2627181A4 (de) 2010-10-13 2011-10-13 Heteroaryle und verwendungen davon

Country Status (23)

Country Link
US (2) US8765746B2 (de)
EP (1) EP2627181A4 (de)
JP (1) JP2013542941A (de)
KR (1) KR20140091462A (de)
CN (1) CN103237450A (de)
AR (1) AR083450A1 (de)
AU (1) AU2011316016A1 (de)
BR (1) BR112013009166A2 (de)
CA (1) CA2814688A1 (de)
CL (1) CL2013001009A1 (de)
CO (1) CO6801713A2 (de)
CR (1) CR20130204A (de)
DO (1) DOP2013000082A (de)
EA (1) EA201390539A1 (de)
EC (1) ECSP13012621A (de)
IL (1) IL225607A0 (de)
MA (1) MA34652B1 (de)
MX (1) MX2013004003A (de)
PE (1) PE20141044A1 (de)
SG (1) SG189396A1 (de)
TW (1) TW201307309A (de)
UY (1) UY33671A (de)
WO (1) WO2012051410A2 (de)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2250160B1 (de) 2008-01-25 2015-11-11 Millennium Pharmaceuticals, Inc. Thiophen-derivate und ihre verwendung als phosphatidylinositol 3-kinase (pi3k) inhibitoren
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
CA2750935A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
PE20131304A1 (es) 2010-08-11 2013-11-14 Millennium Pharm Inc Heteroarilos y sus usos
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012021615A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CN103467481B (zh) * 2012-06-07 2016-08-31 上海汇伦生命科技有限公司 二氢吡啶类化合物、其组合物、制备方法和用途
WO2016130501A1 (en) 2015-02-09 2016-08-18 Incyte Corporation Aza-heteroaryl compounds as pi3k-gamma inhibitors
PL3371190T3 (pl) 2015-11-06 2022-11-07 Incyte Corporation Związki heterocykliczne jako inhibitory pi3k-gamma
ES2833955T3 (es) 2016-01-05 2021-06-16 Incyte Corp Piridinas sustituidas con pirazol/imidazol como inhibidores de PI3K-Gamma
WO2017223414A1 (en) 2016-06-24 2017-12-28 Incyte Corporation HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS
US11236128B2 (en) 2017-07-31 2022-02-01 Agency For Science, Technology And Research Method of preparing stapled peptides
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
PT3847175T (pt) 2018-09-05 2024-04-16 Incyte Corp Formas cristalinas de um inibidor da fosfoinositídeo 3-quinase (pi3k)
CN110041349B (zh) * 2019-05-15 2021-06-01 湖南科技大学 一种含螺二氢嘧啶衍生物及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006046031A1 (en) * 2004-10-25 2006-05-04 Piramed Limited Pharmaceutical compounds
WO2009122148A1 (en) * 2008-03-31 2009-10-08 Ucb Pharma S.A. Fused thiophene and thiazole derivatives as pi3k kinase inhibitors

Family Cites Families (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE581861A (de) 1958-08-20
US3852293A (en) 1972-06-21 1974-12-03 Uniroyal Inc 4-phenyl-2-(3-pyridyl)-thiazole carboxamides
US3821384A (en) 1972-10-06 1974-06-28 Uniroyal Inc Pharmaceutical compositions containing a4-aryl-2-(3-pyridyl)thiazole and methods of using same
DE3021590A1 (de) 1980-06-09 1981-12-17 Hoechst Ag, 6000 Frankfurt 4-halogen-5-(halogenmethyl-phenyl)-oxazol-derivate, ein verfahren zu ihrer herstellung und sie enthaltenden strahlungsempfindliche massen
DD275870A1 (de) 1988-09-27 1990-02-07 Univ Leipzig Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
EP0923579A1 (de) 1996-08-27 1999-06-23 Novartis AG Herbizide s-substituierte 1,2,4,6-thiatriazine
JPH1087490A (ja) 1996-09-10 1998-04-07 Sagami Chem Res Center インターロイキン６生産抑制剤、骨吸収抑制剤、抗骨粗鬆症剤、及びチアゾール化合物
PT853083E (pt) 1997-01-06 2001-12-28 Pfizer Composto de piridilfurano e piridiltiofeno e sua utilizacao farmaceutica
BR9804865B1 (pt) 1997-04-24 2011-08-23 pesticida 3-(fenil substituìdo)-5-(tienil ou furil)-1,2,4-triazóis, composição para controlar insetos ou ácaros, bem como processo para controlar insetos, ácaros, moscas brancas e afìdios, para proteger plantas de afìdios, ácaros ou insetos.
JP2002520324A (ja) 1998-07-10 2002-07-09 メルク エンド カムパニー インコーポレーテッド 新規な血管形成インヒビター
DE19858192A1 (de) 1998-12-17 2000-06-21 Aventis Cropscience Gmbh 4-Trifluormethyl-3-oxazolylpyridine, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung als Schädlingsbekämpfungsmittel
CO5170501A1 (es) 1999-04-14 2002-06-27 Novartis Ag AZOLES SUSTITUIDOS UTILES PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR TNFa eIL-1 Y ENFERMEDADES DEL METABOLISMO OSEO
PT1251848E (pt) 2000-01-18 2004-10-29 Vertex Pharma Inibidores de girase e as sua utilizacoes
JP2004535381A (ja) 2001-04-13 2004-11-25 バーテックス　ファーマシューティカルズ　インコーポレイテッド ｃ−ＪｕｎＮ末端キナーゼ（ＪＮＫ）および他のプロテインキナーゼのインヒビター
WO2002088107A1 (en) 2001-04-26 2002-11-07 Eisai Co., Ltd. Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof
US7405235B2 (en) 2001-05-04 2008-07-29 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
PL210475B1 (pl) 2001-08-13 2012-01-31 Janssen Pharmaceutica Nv Pochodna 2,4,5-tripodstawionego tiazolilu, sposób jej wytwarzania i zastosowanie oraz kompozycja farmaceutyczna i sposób jej wytwarzania
DE60228098D1 (de) 2001-09-05 2008-09-18 Smithkline Beecham Plc Pyridin-substituierte furanderivate als raf-kinase inhibitoren
WO2003027107A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors
US20040198773A1 (en) 2001-09-26 2004-10-07 Barry Hart Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors
NZ533107A (en) 2001-11-08 2007-04-27 Upjohn Co N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives
EP1546137A1 (de) 2002-08-08 2005-06-29 SmithKline Beecham Corporation Benzimidazol-1-yl-thiophen-verbindungen zur behandlung von krebs
AU2003265394A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors containing dimethyl-cyclobutane and methods of their synthesis and use
AU2003265395A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
US6984652B2 (en) 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
WO2005074642A2 (en) 2004-01-30 2005-08-18 Smithkline Beecham Corporation Chemical compounds
RU2006138036A (ru) 2004-03-30 2008-05-10 Чирон Корпорейшн (Us) Производные замещенного тиофена в качестве противораковых средств
JP2008503446A (ja) 2004-05-06 2008-02-07 プレキシコン，インコーポレーテッド Ｐｄｅ４ｂ阻害剤及びその使用
US20080045492A1 (en) 2004-12-21 2008-02-21 Coleman Paul J Mitotic Kinesin Inhibitors
WO2006077428A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
GB0503962D0 (en) 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
CN1834095B (zh) 2005-03-18 2011-04-20 中国科学院上海药物研究所 一类非核苷类抗病毒抑制剂及其制备方法和用途
CN101142217B (zh) 2005-03-21 2010-12-08 伊莱利利公司 咪唑并哒嗪化合物
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
GB0508471D0 (en) * 2005-04-26 2005-06-01 Celltech R&D Ltd Therapeutic agents
DE102005000046A1 (de) 2005-04-28 2006-11-02 Voith Patent Gmbh Maschine zur Herstellung einer Faserstoffbahn
CA2613522A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Imidazole based lxr modulators
KR20080066938A (ko) 2005-10-07 2008-07-17 깃세이 야쿠힌 고교 가부시키가이샤 질소 함유 복소환 화합물 및 그것을 함유하는 의약 조성물
JP2007197324A (ja) 2006-01-23 2007-08-09 Toray Ind Inc ２，４，５−置換−１，３−アゾール誘導体
CA2637933C (en) 2006-01-24 2013-03-12 Eli Lilly And Company Indole sulfonamide modulators of progesterone receptors
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
CN101410387B (zh) 2006-03-27 2013-12-18 内尔维阿诺医学科学有限公司 作为激酶抑制剂的吡啶基-和嘧啶基-取代的吡咯-、噻吩-和呋喃-衍生物
ATE471940T1 (de) 2006-04-26 2010-07-15 Hoffmann La Roche Thienoä3,2-düpyrimidin-derivat geeignet als pi3k inhibitor
WO2007129044A1 (en) 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
EP2439206A1 (de) 2006-05-23 2012-04-11 Vertex Pharmaceuticals Incorporated Thiophencarboxamide als Proteinkinaseninhibitoren
WO2007138110A2 (en) 2006-06-01 2007-12-06 Devgen N.V. Compounds that interact with ion channels, in particular with ion channels from the kv family
EP2035436B1 (de) * 2006-06-26 2011-05-25 UCB Pharma S.A. Kondensierte thiazol-derivate als kinasehemmer
WO2008011560A2 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
WO2008014238A2 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
MX2009001767A (es) 2006-08-14 2009-02-25 Schering Corp Procedimiento e intermediarios para la sintesis de derivados de 2-(quinolin-5-il)-4,5-azol-disustituido.
MX2009002046A (es) 2006-08-24 2009-03-06 Astrazeneca Ab Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos.
WO2008024980A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives
EP2076515B1 (de) 2006-09-20 2013-07-17 Eli Lilly And Company Thiophenpyrazolopyrimidinverbindungen
ES2363178T3 (es) 2006-12-04 2011-07-26 Astrazeneca Ab Compuestos de urea policíclicos antibacterianos.
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
US8207196B2 (en) 2007-02-02 2012-06-26 Baylor College Of Medicine Compositions and methods for the treatment of metabolic disorders
JP5363997B2 (ja) 2007-02-07 2013-12-11 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ａｋｔ活性の阻害剤
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
CL2008001234A1 (es) 2007-04-30 2008-09-22 Genentech Inc Compuestos derivados de heterociclos nitrogenados, inhibidores de las proteinas de apoptosis; y uso en el tratamiento del cancer.
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
WO2008157273A1 (en) 2007-06-14 2008-12-24 Smithkline Beecham Corporation Chemical compounds
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
US8067613B2 (en) 2007-07-16 2011-11-29 Abbott Laboratories Benzimidazole poly(ADP ribose)polymerase inhibitors
WO2009040730A2 (en) 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
CN101932587A (zh) 2007-09-24 2010-12-29 吉宁特有限公司 噻唑并嘧啶pi3k抑制剂化合物及使用方法
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
EP2250160B1 (de) 2008-01-25 2015-11-11 Millennium Pharmaceuticals, Inc. Thiophen-derivate und ihre verwendung als phosphatidylinositol 3-kinase (pi3k) inhibitoren
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
CA2719032C (en) * 2008-03-31 2016-11-08 Steven Do Benzopyran and benzoxepin pi3k inhibitor compounds and methods of use
NZ589844A (en) 2008-06-19 2012-11-30 Millennium Pharm Inc Thiophene or thiazole derivatives and their use as phosphatidylinositol 3-kinase (PI3K) inhibitors
EP2303852A4 (de) 2008-06-26 2011-12-28 Glaxosmithkline Llc Hemmer der akt-aktivität
GB0812309D0 (en) 2008-07-03 2008-08-13 Ucb Pharma Sa Therapeutic agents
EP2310384B1 (de) 2008-07-09 2014-04-09 Merck Sharp & Dohme Corp. Januskinase-hemmer
CN102171196B (zh) 2008-08-04 2015-03-25 默沙东公司 用作脂肪酸酰胺水解酶的抑制剂的*唑衍生物
EP2382207B1 (de) 2008-11-11 2015-04-29 Xcovery Holding Company LLC Inhibitoren der pi3k/mtor-kinase
GB0820819D0 (en) 2008-11-13 2008-12-24 Sareum Ltd Pharmaceutical compounds
WO2010080873A1 (en) 2009-01-08 2010-07-15 Glaxo Group Limited Oxazoles as modulators of chemokine receptors
CA2750935A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
EP2430013B1 (de) 2009-05-13 2014-10-15 Amgen Inc. Heteraryl verbindungen als pikk hemmer
US20110021531A1 (en) 2009-07-27 2011-01-27 Chobanian Harry Oxazole derivatives useful as inhibitors of faah
JP2012254939A (ja) 2009-10-07 2012-12-27 Astellas Pharma Inc オキサゾール化合物
WO2012021615A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
PE20131304A1 (es) 2010-08-11 2013-11-14 Millennium Pharm Inc Heteroarilos y sus usos
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US20130165472A1 (en) 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006046031A1 (en) * 2004-10-25 2006-05-04 Piramed Limited Pharmaceutical compounds
WO2009122148A1 (en) * 2008-03-31 2009-10-08 Ucb Pharma S.A. Fused thiophene and thiazole derivatives as pi3k kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MARK E. WELKER ET AL: "Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 21, no. 14, 1 July 2013 (2013-07-01), pages 4063 - 4091, XP055085671, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2013.04.083 *

Also Published As

Publication number Publication date
BR112013009166A2 (pt) 2016-07-26
ECSP13012621A (es) 2013-07-31
CA2814688A1 (en) 2012-04-19
EA201390539A1 (ru) 2013-09-30
IL225607A0 (en) 2013-06-27
WO2012051410A3 (en) 2012-07-26
DOP2013000082A (es) 2013-10-31
TW201307309A (zh) 2013-02-16
SG189396A1 (en) 2013-05-31
MX2013004003A (es) 2013-10-01
MA34652B1 (fr) 2013-11-02
US20150148334A1 (en) 2015-05-28
US20120214794A1 (en) 2012-08-23
CR20130204A (es) 2013-09-03
UY33671A (es) 2012-04-30
AR083450A1 (es) 2013-02-27
CL2013001009A1 (es) 2013-08-30
CN103237450A (zh) 2013-08-07
JP2013542941A (ja) 2013-11-28
AU2011316016A1 (en) 2013-05-30
WO2012051410A2 (en) 2012-04-19
US8765746B2 (en) 2014-07-01
PE20141044A1 (es) 2014-09-07
KR20140091462A (ko) 2014-07-21
EP2627181A2 (de) 2013-08-21
CO6801713A2 (es) 2013-11-29

Similar Documents

Publication Publication Date Title
HUS2100032I1 (hu) Helyettesített 5-fluor-1H-pirazolopiridin-származékok és alkalmazásuk
SG10201506238SA (en) Heteroaryls And Uses Thereof
IL225607A0 (en) The heteroaryls and their uses
HK1187049A1 (en) Bisaryl-bonded aryltriazolones and use thereof
EP2793879A4 (de) Heteroaryle und verwendungen davon
IL222961A0 (en) Novel dna-dinding proteins and uses thereof
LT3222617T (lt) Psma nukreipti junginiai ir jų naudojimas
EP2640854A4 (de) Nc-rna und verwendung davon
EP2552953A4 (de) Frizzled-bindende stoffe und ihre verwendungen
GB0914644D0 (en) Novel agents and uses thereof
HRP20160922T1 (hr) Oligopeptidni spojevi i njihove uporabe
EP2616468A4 (de) Verschmolzene heteroarlye und anwendungen davon
HRP20182083T1 (hr) Nova kombinacija i uporaba
EP2608785A4 (de) Lipomakrozyklen und deren verwendungen
EP2529013A4 (de) Neuartige beta-glucosidase und verwendungen davon
GB0909768D0 (en) Novel compounds and uses thereof
GB201014319D0 (en) Compounds and uses thereof
EP2638160A4 (de) Nuclione und ribocapside
GB0908087D0 (en) Novel compounds and uses thereof
GB201020268D0 (en) Composition and uses

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20130508

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

AX Request for extension of the european patent

Extension state: BA ME

A4 Supplementary search report drawn up and despatched

Effective date: 20140217

RIC1 Information provided on ipc code assigned before grant

Ipc: A61K 31/365 20060101ALI20140211BHEP

Ipc: A61K 31/35 20060101ALI20140211BHEP

Ipc: A01N 43/16 20060101ALI20140211BHEP

Ipc: A01N 43/78 20060101AFI20140211BHEP

Ipc: A61K 31/425 20060101ALI20140211BHEP

REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1188907

Country of ref document: HK

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN

18D Application deemed to be withdrawn

Effective date: 20160503

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1188907

Country of ref document: HK